Literature DB >> 17496888

Diarylquinolines target subunit c of mycobacterial ATP synthase.

Anil Koul1, Najoua Dendouga, Karen Vergauwen, Brenda Molenberghs, Luc Vranckx, Rudy Willebrords, Zorica Ristic, Holger Lill, Ismet Dorange, Jerome Guillemont, Dirk Bald, Koen Andries.   

Abstract

The diarylquinoline R207910 (TMC207) is a promising candidate in clinical development for the treatment of tuberculosis. Though R207910-resistant mycobacteria bear mutations in ATP synthase, the compound's precise target is not known. Here we establish by genetic, biochemical and binding assays that the oligomeric subunit c (AtpE) of ATP synthase is the target of R207910. Thus targeting energy metabolism is a new, promising approach for antibacterial drug discovery.

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Year:  2007        PMID: 17496888     DOI: 10.1038/nchembio884

Source DB:  PubMed          Journal:  Nat Chem Biol        ISSN: 1552-4450            Impact factor:   15.040


  162 in total

Review 1.  The chemical biology of new drugs in the development for tuberculosis.

Authors:  Clifton E Barry; John S Blanchard
Journal:  Curr Opin Chem Biol       Date:  2010-05-07       Impact factor: 8.822

Review 2.  The challenge of new drug discovery for tuberculosis.

Authors:  Anil Koul; Eric Arnoult; Nacer Lounis; Jerome Guillemont; Koen Andries
Journal:  Nature       Date:  2011-01-27       Impact factor: 49.962

Review 3.  TMC207: the first compound of a new class of potent anti-tuberculosis drugs.

Authors:  Alberto Matteelli; Anna Cc Carvalho; Kelly E Dooley; Afranio Kritski
Journal:  Future Microbiol       Date:  2010-06       Impact factor: 3.165

Review 4.  The c-Ring of the F1FO-ATP Synthase: Facts and Perspectives.

Authors:  Salvatore Nesci; Fabiana Trombetti; Vittoria Ventrella; Alessandra Pagliarani
Journal:  J Membr Biol       Date:  2015-11-30       Impact factor: 1.843

5.  In vitro antimycobacterial spectrum of a diarylquinoline ATP synthase inhibitor.

Authors:  Emma Huitric; Peter Verhasselt; Koen Andries; Sven E Hoffner
Journal:  Antimicrob Agents Chemother       Date:  2007-08-20       Impact factor: 5.191

Review 6.  ATP synthase and the actions of inhibitors utilized to study its roles in human health, disease, and other scientific areas.

Authors:  Sangjin Hong; Peter L Pedersen
Journal:  Microbiol Mol Biol Rev       Date:  2008-12       Impact factor: 11.056

7.  The protonmotive force is required for maintaining ATP homeostasis and viability of hypoxic, nonreplicating Mycobacterium tuberculosis.

Authors:  Srinivasa P S Rao; Sylvie Alonso; Lucinda Rand; Thomas Dick; Kevin Pethe
Journal:  Proc Natl Acad Sci U S A       Date:  2008-08-12       Impact factor: 11.205

Review 8.  New antituberculous drugs derived from natural products: current perspectives and issues in antituberculous drug development.

Authors:  Masayuki Igarashi; Yoshimasa Ishizaki; Yoshiaki Takahashi
Journal:  J Antibiot (Tokyo)       Date:  2017-11-01       Impact factor: 2.649

9.  ATP synthases: bioinformatic based insights into how their electrochemically driven motor comprised of subunits a and c might serve as a drug target.

Authors:  Masatomo Maeda
Journal:  J Bioenerg Biomembr       Date:  2008-04-23       Impact factor: 2.945

10.  Selectivity of TMC207 towards mycobacterial ATP synthase compared with that towards the eukaryotic homologue.

Authors:  Anna C Haagsma; Rooda Abdillahi-Ibrahim; Marijke J Wagner; Klaas Krab; Karen Vergauwen; Jerome Guillemont; Koen Andries; Holger Lill; Anil Koul; Dirk Bald
Journal:  Antimicrob Agents Chemother       Date:  2008-12-15       Impact factor: 5.191

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